Amity Institute of Biotechnology, Amity University Uttar Pradesh, Sector-125, NOIDA-201313, India.
Amity Institute of Microbial Biotechnology, Amity University Uttar Pradesh, Sector-125, NOIDA-201313, India.
Int J Biol Macromol. 2020 Dec 1;164:45-52. doi: 10.1016/j.ijbiomac.2020.07.086. Epub 2020 Jul 15.
Nanotechnology based antimicrobial drugs are developed to enhance their properties to combat multidrug resistant microbes. Carbenoxolone (CBX) is a semi-synthetic derivate of a natural substance from the licorice plant, with anti- (inflammatory, fungal, viral, microbial, fibrotic and cancer) properties. Though used to treat gastric ulcers, its low aqueous stability, low bioavailability and toxicity limited the drug's utility. To enhance its antimicrobial activity and reduce cytotoxicity, a controlled release nanoformulation was developed using natural biodegradable polymer chitosan (CS) as a carrier which is biocompatible, nontoxic with placid antimicrobial property. UV-visible spectroscopy, electron microscopy, and Fourier transform infrared spectroscopy were used for characterization of the resultant CS-CBX nanoparticles (NPs). They were spherical with uniform dispersion, ~200 nm in size with surface charge of +18.6 mV and drug encapsulation of >80%. Drug release kinetics exhibited a controlled release of 86% over 36 h following zero order kinetics. The anti-microbial activity against common pathogenic Gram -ve and +ve bacteria and yeast increased ~2-fold with a concomitant 4-fold reduction in cytotoxicity assessed using human lung adeno carcinoma (A549) cells. This study demonstrates the affirmative aspects of CS-CBX NPs as a promising antibacterial agent and may facilitate repositioning of the drug for diverse applications.
基于纳米技术的抗菌药物被开发出来，以增强其性能，用于对抗多药耐药微生物。卡波氯铵（CBX）是甘草植物中天然物质的半合成衍生物，具有抗炎、抗真菌、抗病毒、抗微生物、抗纤维化和抗癌特性。虽然它被用于治疗胃溃疡，但由于其低水稳定性、低生物利用度和毒性，限制了它的应用。为了提高其抗菌活性和降低细胞毒性，采用天然可生物降解聚合物壳聚糖（CS）作为载体，开发了一种控制释放的纳米制剂，该载体具有生物相容性、无毒性和平稳的抗菌特性。利用紫外-可见光谱、电子显微镜和傅里叶变换红外光谱对所得 CS-CBX 纳米颗粒（NPs）进行了表征。这些 NPs 为球形，具有均匀的分散性，粒径约为 200nm，表面带正电荷 +18.6mV，药物包封率>80%。药物释放动力学表现出零级动力学的 86%的控释，在 36 小时内释放。对常见的致病性革兰氏阴性和阳性细菌和酵母的抗菌活性提高了约 2 倍，同时对人肺腺癌细胞（A549）的细胞毒性降低了 4 倍。本研究证明了 CS-CBX NPs 作为一种有前途的抗菌剂的积极方面，并可能促进该药物重新定位，用于多种应用。
